EP3579828A4 - Co-kristalle von substituierten glycinverbindungen und verwendungen davon - Google Patents

Co-kristalle von substituierten glycinverbindungen und verwendungen davon Download PDF

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Publication number
EP3579828A4
EP3579828A4 EP18751659.6A EP18751659A EP3579828A4 EP 3579828 A4 EP3579828 A4 EP 3579828A4 EP 18751659 A EP18751659 A EP 18751659A EP 3579828 A4 EP3579828 A4 EP 3579828A4
Authority
EP
European Patent Office
Prior art keywords
crystals
substituted glycine
glycine compounds
compounds
substituted
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP18751659.6A
Other languages
English (en)
French (fr)
Other versions
EP3579828A1 (de
EP3579828B1 (de
Inventor
Guochuan Emil Tsai
Ching-Cheng Wang
Tien-Lan HSIEH
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SyneuRx International Taiwan Corp
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SyneuRx International Taiwan Corp
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Publication date
Application filed by SyneuRx International Taiwan Corp filed Critical SyneuRx International Taiwan Corp
Publication of EP3579828A1 publication Critical patent/EP3579828A1/de
Publication of EP3579828A4 publication Critical patent/EP3579828A4/de
Application granted granted Critical
Publication of EP3579828B1 publication Critical patent/EP3579828B1/de
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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13Dicarboxylic acids
    • C07C57/15Fumaric acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/10Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
    • C07C229/12Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of acyclic carbon skeletons
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235Saturated compounds containing more than one carboxyl group
    • C07C59/245Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255Tartaric acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/62Three oxygen atoms, e.g. ascorbic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Medicinal Preparation (AREA)
EP18751659.6A 2017-02-13 2018-01-11 Co-kristalle von substituierten glycinverbindungen und verwendungen davon Active EP3579828B1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15/430,750 US9877942B1 (en) 2017-02-13 2017-02-13 Co-crystals of substituted glycine and uses thereof
PCT/CN2018/072186 WO2018145553A1 (en) 2017-02-13 2018-01-11 Co-crystals of substituted glycine compounds and uses thereof

Publications (3)

Publication Number Publication Date
EP3579828A1 EP3579828A1 (de) 2019-12-18
EP3579828A4 true EP3579828A4 (de) 2020-11-18
EP3579828B1 EP3579828B1 (de) 2025-03-26

Family

ID=61005084

Family Applications (1)

Application Number Title Priority Date Filing Date
EP18751659.6A Active EP3579828B1 (de) 2017-02-13 2018-01-11 Co-kristalle von substituierten glycinverbindungen und verwendungen davon

Country Status (11)

Country Link
US (4) US9877942B1 (de)
EP (1) EP3579828B1 (de)
JP (2) JP2020507567A (de)
KR (1) KR20190118574A (de)
CN (1) CN110520117A (de)
CA (1) CA3051284A1 (de)
IL (1) IL268220B (de)
MX (1) MX393880B (de)
RU (1) RU2019128576A (de)
TW (1) TWI670058B (de)
WO (1) WO2018145553A1 (de)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102403048B1 (ko) * 2016-06-13 2022-05-26 신유알엑스 인터내셔널 (타이완) 코포레이션 벤조산나트륨의 공-결정 및 그의 용도
US9877942B1 (en) 2017-02-13 2018-01-30 Syneurx International (Taiwan) Corp. Co-crystals of substituted glycine and uses thereof
CN113233976B (zh) * 2021-05-08 2021-11-16 广州萃普生物科技有限公司 一种没食子酸和氨基乙酸共晶及含有该共晶的美白膏霜
EP4419499B1 (de) 2021-10-20 2026-02-25 Purac Biochem B.V. Co-kristall von zitronensäure und glycin und verwendungen davon

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6228875B1 (en) * 1998-04-14 2001-05-08 The General Hospital Corporation Methods for treating neuropsychiatric disorders
EP1727520A2 (de) * 2003-12-09 2006-12-06 Medcrystalforms, Llc Verfahren zur herstellung von mischphasen-kokristallen mit wirkstoffen
US20100204204A1 (en) * 2007-06-06 2010-08-12 University Of South Florida Nutraceutical co-crystal compositions
WO2009018368A1 (en) * 2007-07-30 2009-02-05 Los Angeles Biomedical Research Institute At Harbor-Ucla Medical Center Combination treatment of nmda (n-methyl-d-aspartate)-enhancer, glycine transporter inhibitor, d-amino acid oxidase inhibitor (daaoi) for neuropsychiatric disorders
GB201411802D0 (en) * 2014-07-02 2014-08-13 Univ Bradford Effervescent compositions
US9877942B1 (en) 2017-02-13 2018-01-30 Syneurx International (Taiwan) Corp. Co-crystals of substituted glycine and uses thereof

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
M ILCZYSZYN ET AL: "Sarcosine-maleic acid (1:1) crystal: structure, 13C NMR and vibrational properties, protonation character", SPECTROCHIMICA ACTA. PART A: MOLECULAR AND BIOMOLECULAR SPECTROSCOPY, vol. 59, no. 8, 1 June 2003 (2003-06-01), NL, pages 1815 - 1828, XP055732857, ISSN: 1386-1425, DOI: 10.1016/S1386-1425(02)00413-4 *
R. V. KRISHNAKUMAR ET AL: "Sarcosinium tartrate", ACTA CRYSTALLOGRAPHICA SECTION C. CRYSTAL STRUCTURE COMMUNICATIONS, vol. 57, no. 2, 15 February 2001 (2001-02-15), DK, pages 165 - 166, XP055732719, ISSN: 0108-2701, DOI: 10.1107/S0108270100012440 *
SCOTT A SOUTHERN ET AL: "Supporting Information NMR Investigations of Non-Covalent Carbon Tetrel Bonds. Computational Assessment and Initial Experimental Observation Contents", 10 December 2015 (2015-12-10), XP055732365, Retrieved from the Internet <URL:https://pubs.acs.org/doi/suppl/10.1021/acs.jpca.5b10848/suppl_file/jp5b10848_si_001.pdf> [retrieved on 20200921] *
SCOTT A. SOUTHERN ET AL: "NMR Investigations of Noncovalent Carbon Tetrel Bonds. Computational Assessment and Initial Experimental Observation", JOURNAL OF PHYSICAL CHEMISTRY. A, MOLECULES, SPECTROSCOPY,KINETICS, ENVIRONMENT AND GENERAL THEORY, vol. 119, no. 49, 10 December 2015 (2015-12-10), US, pages 11891 - 11899, XP055732362, ISSN: 1089-5639, DOI: 10.1021/acs.jpca.5b10848 *
See also references of WO2018145553A1 *

Also Published As

Publication number Publication date
US10765651B2 (en) 2020-09-08
US9877942B1 (en) 2018-01-30
TW201840308A (zh) 2018-11-16
JP2023082101A (ja) 2023-06-13
WO2018145553A1 (en) 2018-08-16
EP3579828A1 (de) 2019-12-18
MX393880B (es) 2025-03-24
US20180228754A1 (en) 2018-08-16
JP2020507567A (ja) 2020-03-12
US20190262299A1 (en) 2019-08-29
RU2019128576A3 (de) 2021-05-14
KR20190118574A (ko) 2019-10-18
CA3051284A1 (en) 2018-08-16
RU2019128576A (ru) 2021-03-15
EP3579828B1 (de) 2025-03-26
US20180228753A1 (en) 2018-08-16
US10328042B2 (en) 2019-06-25
IL268220B (en) 2022-04-01
US10328041B2 (en) 2019-06-25
CN110520117A (zh) 2019-11-29
JP7723991B2 (ja) 2025-08-15
MX2019009616A (es) 2019-10-14
TWI670058B (zh) 2019-09-01
IL268220A (en) 2019-09-26

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